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Synthesis and SAR of novel parenteral anti-pseudomonal cephalosporins: discovery of FR264205 |
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| Authors: | Toda Ayako Ohki Hidenori Yamanaka Toshio Murano Kenji Okuda Shinya Kawabata Kohji Hatano Kazuo Matsuda Keiji Misumi Keiji Itoh Kenji Satoh Kenji Inoue Satoshi |
| Institution: | aChemistry Research Labs, Astellas Pharma Inc., 2-1-6 Kashima, Yodogawa-ku, Osaka 532-8514, Japan;bPharmacology Research Labs, Astellas Pharma Inc., 2-1-6 Kashima, Yodogawa-ku, Osaka 532-8514, Japan;cInstitute for Medical Research, Wakunaga Pharmaceutical Co. Ltd., 1624 Shimokotachi, Koda-cho, Akitakata-shi, Hiroshima 739-1195, Japan |
| Abstract: | We describe herein the synthesis and biological evaluation of a series of novel cephalosporins with potent activity against Pseudomonas aeruginosa. Introduction of various amino groups to the 4-position of a 3-amino-2-methylpyrazole cephalosporin 3-side chain resulted in enhanced MIC values against multiple Pseudomonas aeruginosa strains and ultimately led to the discovery of FR264205 (15) with excellent anti-bacterial activity and weak convulsion effect by direct intracerebroventricular injection assay. |
| Keywords: | FR264205 Cephalosporin Pseudomonas aeruginosa SAR |
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